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1. 发明申请

US20140206649A1 CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译： CANNABINOID受体调节剂
公开(公告)号：US20140206649A1
公开(公告)日：2014-07-24
申请号：US14001131
申请日：2012-02-24
申请人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Anthony Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
发明人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Anthony Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
IPC分类号： A61K31/675 , A61K31/416 , A61K31/4439 , A61K45/06 , A61K31/497
CPC分类号： A61K31/497 , A61K31/13 , A61K31/416 , A61K31/4439 , A61K31/485 , A61K31/675 , A61K45/06 , C07D231/54 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07F9/65583
摘要： Provided are certain methods useful in the treatment of pain comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;
摘要翻译：提供有用于治疗疼痛的某些方法，包括施用式Ia化合物及其调节大麻素CB 2受体活性的药物组合物;

2. 发明授权

US09597340B2 Cannabinoid receptor modulators 有权
公开(公告)号：US09597340B2
公开(公告)日：2017-03-21
申请号：US14001132
申请日：2012-02-24
申请人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
发明人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
IPC分类号： A61K31/4439 , A61K31/675 , A61K31/416 , A61K45/06 , A61K31/497
CPC分类号： A61K31/675 , A61K31/416 , A61K31/4439 , A61K31/497 , A61K45/06 , A61K2300/00
摘要： Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;

3. 发明申请

US20150126477A1 CANNABINOID RECEPTOR MODULATORS 有权
标题翻译： CANNABINOID受体调节剂
公开(公告)号：US20150126477A1
公开(公告)日：2015-05-07
申请号：US14001132
申请日：2012-02-24
申请人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
发明人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
IPC分类号： A61K31/675 , A61K31/4439 , A61K31/497 , A61K45/06 , A61K31/416
CPC分类号： A61K31/675 , A61K31/416 , A61K31/4439 , A61K31/497 , A61K45/06 , A61K2300/00
摘要： Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;
摘要翻译：提供某些方法可用于治疗癌症，包括施用式Ia化合物及其药物组合物，其调节大麻素CB2受体的活性;

4. 发明授权

US08778950B2 Cannabinoid receptor modulators 有权
标题翻译：大麻素受体调节剂
公开(公告)号：US08778950B2
公开(公告)日：2014-07-15
申请号：US13392074
申请日：2010-08-27
申请人： Robert M. Jones , Sangdon Han , Lars Thoresen , Jae-Kyu Jung , Sonja Strah-Pleynet , Xiuwen Zhu , Yifeng Xiong , Dawei Yue
发明人： Robert M. Jones , Sangdon Han , Lars Thoresen , Jae-Kyu Jung , Sonja Strah-Pleynet , Xiuwen Zhu , Yifeng Xiong , Dawei Yue
IPC分类号： A61K31/4965 , A01N43/56 , A61K31/415 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D231/54 , C07D487/00
CPC分类号： C07D231/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07F9/65583
摘要： The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease.
摘要翻译：本发明涉及某些式Ia化合物及其药物组合物，其调节大麻素CB2受体的活性。本发明还涉及某些式Ia化合物及其药物组合物，其调节CB1受体和CB2受体的活性。本发明的化合物及其药物组合物涉及可用于治疗以下疼痛的方法：疼痛，例如骨和关节疼痛，肌肉疼痛，牙痛，偏头痛和其他头痛疼痛，炎性疼痛，神经性疼痛，疼痛发生于与骨关节炎相关的治疗和疼痛的不利影响; 痛觉过敏异常性疼痛炎性痛觉过敏; 神经性痛觉过敏; 急性伤害感受骨质疏松症多发性硬化相关性痉挛状态; 自身免疫性疾病过敏反应; CNS炎症; 动脉粥样硬化不良免疫细胞活性和炎症; 年龄相关性黄斑变性; 咳嗽; 白血病; 淋巴瘤 CNS肿瘤; 前列腺癌; 阿尔茨海默氏病; 中风引起的损伤; 痴呆; 肌萎缩性侧索硬化和帕金森病。

5. 发明申请

US20130165412A1 CANNABINOID RECEPTOR MODULATORS 有权
标题翻译： CANNABINOID受体调节剂
公开(公告)号：US20130165412A1
公开(公告)日：2013-06-27
申请号：US13616918
申请日：2012-09-14
申请人： Robert M. Jones , Sangdon Han , Lars Thoresen , Jae-Kyu Jung , Sonja Strah-Pleynet , Xiuwen Zhu , Yifeng Xiong , Dawei Yue
发明人： Robert M. Jones , Sangdon Han , Lars Thoresen , Jae-Kyu Jung , Sonja Strah-Pleynet , Xiuwen Zhu , Yifeng Xiong , Dawei Yue
IPC分类号： C07F9/6558 , C07D401/12 , C07D403/12 , C07D413/12 , C07D413/14 , C07D231/54 , C07D403/04
CPC分类号： C07D231/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07F9/65583
摘要： The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease.
摘要翻译：本发明涉及某些式Ia化合物及其药物组合物，其调节大麻素CB2受体的活性。本发明还涉及某些式Ia化合物及其药物组合物，其调节CB1受体和CB2受体的活性。本发明的化合物及其药物组合物涉及可用于治疗以下疼痛的方法：疼痛，例如骨和关节疼痛，肌肉疼痛，牙痛，偏头痛和其他头痛疼痛，炎性疼痛，神经性疼痛，疼痛发生于与骨关节炎相关的治疗和疼痛的不利影响; 痛觉过敏异常性疼痛炎性痛觉过敏; 神经性痛觉过敏; 急性伤害感受骨质疏松症多发性硬化相关性痉挛状态; 自身免疫性疾病过敏反应; CNS炎症; 动脉粥样硬化不良免疫细胞活性和炎症; 年龄相关性黄斑变性; 咳嗽; 白血病; 淋巴瘤 CNS肿瘤; 前列腺癌; 阿尔茨海默氏病; 中风引起的损伤; 痴呆; 肌萎缩性侧索硬化和帕金森病。

6. 发明申请

US20120214766A1 CANNABINOID RECEPTOR MODULATORS 有权
标题翻译： CANNABINOID受体调节剂
公开(公告)号：US20120214766A1
公开(公告)日：2012-08-23
申请号：US13392074
申请日：2010-08-27
申请人： Robert M. Jones , Sangdon Han , Lars Thoresen , Jae-Kyu Jung , Sonja Strah-Pleynet , Xiuwen Zhu , Yifeng Xiong , Dawei Yue
发明人： Robert M. Jones , Sangdon Han , Lars Thoresen , Jae-Kyu Jung , Sonja Strah-Pleynet , Xiuwen Zhu , Yifeng Xiong , Dawei Yue
IPC分类号： A61K31/416 , A61P19/02 , C07D231/54 , C07D413/06 , A61K31/5377 , C07D401/12 , A61K31/4439 , C07D401/04 , C07D403/04 , A61K31/497 , C07D413/12 , C07D413/14 , A61K31/501 , C07D409/04 , C07D403/12 , C07D401/14 , C07D405/12 , C07D405/14 , A61K31/454 , C07F9/6558 , A61K31/675 , A61P29/00
CPC分类号： C07D231/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07F9/65583
摘要： The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease.
摘要翻译：本发明涉及某些式Ia化合物及其药物组合物，其调节大麻素CB2受体的活性。本发明还涉及某些式Ia化合物及其药物组合物，其调节CB1受体和CB2受体的活性。本发明的化合物及其药物组合物涉及可用于治疗以下疼痛的方法：疼痛，例如骨和关节疼痛，肌肉疼痛，牙痛，偏头痛和其他头痛疼痛，炎性疼痛，神经性疼痛，疼痛发生于与骨关节炎相关的治疗和疼痛的不利影响; 痛觉过敏异常性疼痛炎性痛觉过敏; 神经性痛觉过敏; 急性伤害感受骨质疏松症多发性硬化相关性痉挛状态; 自身免疫性疾病过敏反应; CNS炎症; 动脉粥样硬化不良免疫细胞活性和炎症; 年龄相关性黄斑变性; 咳嗽; 白血病; 淋巴瘤 CNS肿瘤; 前列腺癌; 阿尔茨海默氏病; 中风引起的损伤; 痴呆; 肌萎缩性侧索硬化和帕金森病。

7. 发明申请

US20140135345A1 CRYSTALLINE FORMS AND PROCESSES FOR THE PREPARATION OF CANNABINOID RECEPTOR MODULATORS 有权
标题翻译：用于制备CANNABINOID受体调节剂的晶体形式和方法
公开(公告)号：US20140135345A1
公开(公告)日：2014-05-15
申请号：US14001133
申请日：2012-02-24
申请人： Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter
发明人： Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter
IPC分类号： C07D403/04
CPC分类号： C07D403/04 , A61K31/497 , A61P29/00 , C07B2200/13
摘要： The present invention relates to crystalline forms of (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)-1-hydroxymethyl-2,2-dimethyl-propyl)-amide (Compound 1) and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor and are therefore useful in the treatment of CB2 receptor-mediated disorders, for example, osteoarthritis; pain; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation for example; atherosclerosis; undesired immune cell activity, and inflammation associated with a disorder selected from: osteoarthritis, anaphylaxis, Behcet's disease, graft rejection, vasculitis, gout, spondylitis, viral disease, bacterial disease, lupus, inflammatory bowel disease, autoimmune hepatitis, and type 1 diabetes mellitus; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis; and Parkinson's disease.
摘要翻译：本发明涉及（1aS，5aS）-2-（4-氧 - 吡嗪-2-基）-1a，2,5,5a-四氢-1H-2,3-二氮杂 - 环丙烷[a] 顺式-4-羧酸（（S）-1-羟甲基-2,2-二甲基 - 丙基） - 酰胺（化合物1）及其药物组合物，其调节大麻素CB2受体的活性，因此可用于治疗 CB2受体介导的病症，例如骨关节炎; 疼痛; 痛觉过敏异常性疼痛炎性痛觉过敏; 神经性痛觉过敏; 急性伤害感受骨质疏松症多发性硬化相关性痉挛状态; 自身免疫性疾病过敏反应; CNS炎症例如; 动脉粥样硬化不良免疫细胞活性和与选自以下的疾病相关的炎症：骨关节炎，过敏反应，贝切特氏病，移植排斥反应，血管炎，痛风，脊椎炎，病毒性疾病，细菌性疾病，狼疮，炎性肠病，自身免疫性肝炎和1型糖尿病 ; 年龄相关性黄斑变性; 咳嗽; 白血病; 淋巴瘤 CNS肿瘤; 前列腺癌; 阿尔茨海默氏病; 中风引起的损伤; 痴呆; 肌萎缩性侧索硬化; 和帕金森病。

8. 发明授权

US09458136B2 Crystalline forms and processes for the preparation of cannabinoid receptor modulators 有权
标题翻译：用于制备大麻素受体调节剂的结晶形式和方法
公开(公告)号：US09458136B2
公开(公告)日：2016-10-04
申请号：US14001133
申请日：2012-02-24
申请人： Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter
发明人： Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter
IPC分类号： A61K31/4965 , C07D403/04 , A61K31/497
CPC分类号： C07D403/04 , A61K31/497 , A61P29/00 , C07B2200/13
摘要： The present invention relates to crystalline forms of (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)-1-hydroxymethyl-2,2-dimethyl-propyl)-amide (Compound 1) and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor and are therefore useful in the treatment of CB2 receptor-mediated disorders, for example, osteoarthritis; pain; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation for example; atherosclerosis; undesired immune cell activity, and inflammation associated with a disorder selected from: osteoarthritis, anaphylaxis, Behcet's disease, graft rejection, vasculitis, gout, spondylitis, viral disease, bacterial disease, lupus, inflammatory bowel disease, autoimmune hepatitis, and type 1 diabetes mellitus; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis; and Parkinson's disease.
摘要翻译：本发明涉及（1aS，5aS）-2-（4-氧 - 吡嗪-2-基）-1a，2,5,5a-四氢-1H-2,3-二氮杂 - 环丙烷[a] 顺式-4-羧酸（（S）-1-羟甲基-2,2-二甲基 - 丙基） - 酰胺（化合物1）及其药物组合物，其调节大麻素CB2受体的活性，因此可用于治疗 CB2受体介导的疾病，例如骨关节炎; 疼痛; 痛觉过敏异常性疼痛炎性痛觉过敏; 神经性痛觉过敏; 急性伤害感受骨质疏松症多发性硬化相关性痉挛状态; 自身免疫性疾病过敏反应; CNS炎症例如; 动脉粥样硬化不良免疫细胞活性和与选自以下的疾病相关的炎症：骨关节炎，过敏反应，贝切特氏病，移植排斥反应，血管炎，痛风，脊椎炎，病毒性疾病，细菌性疾病，狼疮，炎性肠病，自身免疫性肝炎和1型糖尿病 ; 年龄相关性黄斑变性; 咳嗽; 白血病; 淋巴瘤 CNS肿瘤; 前列腺癌; 阿尔茨海默氏病; 中风引起的损伤; 痴呆; 肌萎缩性侧索硬化; 和帕金森病。

9. 发明申请

US20140066369A1 Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto 审中-公开
标题翻译： GPR119受体的调节剂和与之相关的疾病的治疗
公开(公告)号：US20140066369A1
公开(公告)日：2014-03-06
申请号：US14112384
申请日：2012-04-18
申请人： Robert M. Jones , Daniel J. Buzard , Sangdon Han , Sun Hee Kim , Juerg Lehmann , Dawei Yue , Xiuwen Zhu
发明人： Robert M. Jones , Daniel J. Buzard , Sangdon Han , Sun Hee Kim , Juerg Lehmann , Dawei Yue , Xiuwen Zhu
IPC分类号： C07D295/205 , A61K45/06 , C07D239/42 , A61K31/506 , A61K31/496 , A61K31/499 , C07D249/08 , C07D403/12 , C07D257/04 , C07D487/08 , A61K31/4995 , C07D241/38 , A61K31/495 , C07D271/07
CPC分类号： C07D295/205 , A61K31/495 , A61K31/496 , A61K31/499 , A61K31/4995 , A61K31/506 , A61K45/06 , C07D207/325 , C07D213/68 , C07D213/71 , C07D213/85 , C07D231/12 , C07D233/60 , C07D239/34 , C07D239/42 , C07D241/04 , C07D241/08 , C07D241/38 , C07D249/06 , C07D249/08 , C07D249/10 , C07D257/04 , C07D271/06 , C07D271/07 , C07D295/21 , C07D295/26 , C07D305/08 , C07D401/12 , C07D403/12 , C07D471/08 , C07D487/08
摘要： The present invention relates to compounds of Formula I and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
摘要翻译：本发明涉及式I化合物及其药学上可接受的盐，溶剂合物和水合物，其可用作单一药剂或与一种或多种另外的药剂组合使用，例如DPP-IV抑制剂，双胍类， α-葡糖苷酶抑制剂，胰岛素类似物，磺酰脲类，SGLT2抑制剂，氯噻嗪，噻唑烷二酮或抗糖尿病肽类似物，在治疗中例如选自：GPR119-受体相关病症 ; 通过增加血液肠降血糖水平来改善病情; 以低骨量为特征的病症; 神经障碍代谢相关疾病; 2型糖尿病; 肥胖; 和相关的并发症。

10. 发明授权

US08785441B2 3-phenyl-pyrazole derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto 有权
标题翻译： 3-苯基 - 吡唑衍生物作为可用于治疗与之相关疾病的5-HT2A 5-羟色胺受体的调节剂
公开(公告)号：US08785441B2
公开(公告)日：2014-07-22
申请号：US13616842
申请日：2012-09-14
申请人： Bradley Teegarden , Yifeng Xiong , Sonja Strah-Pleynet , Honnappa Jayakumar , Peter I. Dosa , Konrad Feichtinger , Martin Casper , Juerg Lehmann , Robert M. Jones , David J. Unett , Jin Sun Karoline Choi
发明人： Bradley Teegarden , Yifeng Xiong , Sonja Strah-Pleynet , Honnappa Jayakumar , Peter I. Dosa , Konrad Feichtinger , Martin Casper , Juerg Lehmann , Robert M. Jones , David J. Unett , Jin Sun Karoline Choi
IPC分类号： A61K31/4155 , C07D413/10
CPC分类号： C07D231/12 , A61K31/5377 , C07D231/16 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D487/08
摘要： The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.
摘要翻译：本发明涉及式（Ia）的某些3-苯基 - 吡唑衍生物及其药物组合物，其调节5-HT2A 5-羟色胺受体的活性。化合物及其药物组合物涉及可用于治疗血小板聚集，冠状动脉疾病，心肌梗死，短暂性脑缺血发作，心绞痛，中风，心房颤动，降低血块形成风险，哮喘或其症状，激动或症状，行为障碍，药物诱导的精神病，兴奋性精神病，吉列斯图雷特综合征，躁狂症，有机或非精神病精神病，精神病，精神病，急性精神分裂症，慢性精神分裂症，精神分裂症精神分裂症和相关疾病，以及睡眠障碍，睡眠障碍，糖尿病相关病症，进行性多灶性脑白质病等。本发明还涉及与单独或一起施用的其它药剂组合治疗5-HT2A 5-羟色胺受体介导的病症的方法。

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